Home NF-κB IκB/IKK inhibitor - Apoptosis related activator - DUB inhibitor BAY 11-7082 For research use only.

BAY 11-7082

Synonyms: BAY 11-7821

BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.

BAY 11-7082 Chemical Structure

BAY 11-7082 Chemical Structure

CAS: 19542-67-7

Selleck's BAY 11-7082 has been cited by 347 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa Function Assay 10 μM 1.5 h abolishes BPA induced up regulation of FN and MMP-9  25797437
SiHa  Function Assay 10 μM 1.5 h abolishes BPA induced up regulation of FN and MMP-9  25797437
ARPE-19 Function Assay 1 μM 0.5 h suppresses TG-induced IL-8 promoter activation 25593029
HCT116 Function Assay 5 μM 2 h DMSO attenuates silymarin-induced downregulation of cyclin D1 25479723
HMECs Function Assay 5 μM 2 h abolishes TNF-α-induced VCAM-1 expression  25193116
A549  Function Assay 10 µM 12 h suppresses Dvl-3 induced activation of p65 25156800
RAW 264.7 Function Assay 5 μM 1 h inhibits TNF-α and IL-12 p40 production 25019567
macrophages Function Assay 5 µM 3 h partially blocks YPFS-induced expression of iNOS and COX-2  24967898
HUVECs Function Assay 3-30 μM 1 h reduces the expression of miR-146a in a dose-dependent manner 24863965
HeLa  Function Assay 5 μM 24 h DMSO reduces the activity of TNF-α promoter  24657783
A549 Function Assay 10 μM 1 h inhibits the increase of phospho-IκBα in PA103-infected cultures  24612488
HUVEC Function Assay 20 µM 0.5 h DMSO prevents the induction of EAM expression 24551209
A549RT-eto Apoptosis Assay 10 μM 24 h DMSO accelerates FERO-mediated apoptosis 24535083
THP-1  Function Assay 0.1/1 μM 0.5 h abrogates TNF-α secretion as well as the increased secretion of IL-6 and IL-1β 24378536
SKCXCR2  Growth Inhibition Assay 2 µM 48 h decreases cell proliferation significantly 24376747
SKCXCR2  Function Assay 2 µM 48 h blocks the CXCL1-induced cell invasion 24376747
OVCXCR2 Function Assay 2 µM 48 h blocks the CXCL1-induced cell invasion 24376747
DSCs  Function Assay 2.5 μM 0.5 h reverses the enhancement of CCL2/CCR2 expression of DSCs induced by IL-33 24344240
WPs Function Assay 25 μM 5 min suppresses ATP and vWF secretion 24331207
A549RT-eto Apoptosis Assay 10 μM 24 h accelerates F14 extract-mediated apoptosis combined treatment with F14 24220725
A549RT-eto Function Assay 10 μM 24 h decreases the expression levels of NF-κB and P-gp  24220725
FaDu Function Assay 2 h inhibits p65 expression and blocks TNFα-induced TWIST expression 24220622
IVD  Function Assay 10 μM 3 d reverses TNF-α–mediated suppression of the disc matrix macromolecules aggrecan and collagen II 24176808
IVD  Function Assay 10 μM 3 d abrogates TNF-α–induced up-regulation of ADAMTS-4 and ADAMTS-5  24176808
iNKT Function Assay 10/100 μM 0.5 h inhibits the induction of A2AR mRNA and other factor 24124453
PC-3 Function Assay 2.5/5/10 μM 0.5 h blocks IGF-II-induced STS mRNA expression  24055520
THP-1  Function Assay 10 μM 1 h abolishes the effect of rHSP27 on SR-A mRNA 23939398
A549 Function Assay 1 μM 48 h enhances the up-regulation of IκB and subsequent decrease in Bax expression induced by combined stimulation 23900080
A549 Apoptosis Assay 1 μM 48 h reduces the cell death induced by combined stimulation 23900080
NCI-N87 Growth Inhibition Assay 10/20/30 μM 6/24 h suppresses cell viability significantly 23846545
AGS Growth Inhibition Assay 10/20/30 μM 6/24 h suppresses cell viability significantly 23846545
MGC80-3 Growth Inhibition Assay 10/20/30 μM 6/24 h suppresses cell viability significantly 23846545
HGC-27  Function Assay 7.5/15/30 μM 6 h induces the dephosphorylation and up-regulation of IκBα 23846545
MGC80-3 Function Assay 7.5/15/30 μM 6 h induces the dephosphorylation and up-regulation of IκBα 23846545
HGC-27  Apoptosis Assay 7.5/15/30 μM 6 h induces apoptosis in a time- and dose-dependent manner 23846545
HBE  Function Assay 10μM 3h abolishes the increases of IL-6 expression induced by CSE 23824089
HepG2 Function Assay 0.3/1/3 μM 48 h reduces IL6-induced PON1 expression 23791833
THP-1 Function Assay 5 µM 1 h DMSO inhibits MTB-induced NFκB activation 23634218
THP-1  Growth Inhibition Assay 5 µM 4/8 d DMSO reduces the viability of intracellular MTB 23634218
MDM Growth Inhibition Assay 5 µM 4/8 d DMSO reduces the viability of intracellular MTB 23634218
AM Growth Inhibition Assay 5 µM 4/8 d DMSO reduces the viability of intracellular MTB 23634218
RAW 264  Function Assay 0.2-5 µM 30/60/90 min inhibits the phosphatase activity of PTP1B  23578302
HUVEC Function Assay 10 μM 0.5 h DMSO counteractes the loss of Tie2 mRNA 23563632
HT29 Function Assay 10/30/100 μM 1 h inhibites both TWEAK-induced p100 processing 23527154
HT29 Function Assay 10/30/100 μM 1 h inhibits TNF-induced phosphorylation and degradation of IκBα 23527154
MM.1S Apoptosis Assay 30 µM 3 h induces MM cell death involves necrosis 23527154
KMS-12-BM Apoptosis Assay 30 µM 3 h induces MM cell death involves necrosis 23527154
BAFs Function Assay 0.5/1 μM 24 h inhibits TNFα/DEX induced CYP19A1 transcripts 23485457
SP6.5 Function Assay 5 μM 2 h decreases translocation of p65 in the nucleus  23443086
VUP Function Assay 5 μM 2 h decreases translocation of p65 in the nucleus  23443086
OCM1 Function Assay 5 μM 2 h decreases translocation of p65 in the nucleus  23443086
OM431 Function Assay 5 μM 2 h decreases translocation of p65 in the nucleus  23443086
SP6.5 Growth Inhibition Assay 2.5-20 μM 24 h  IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner 23443086
VUP Growth Inhibition Assay 2.5-20 μM 24 h  IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner 23443086
OCM1 Growth Inhibition Assay 2.5-20 μM 24 h  IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner 23443086
OM431 Growth Inhibition Assay 2.5-20 μM 24 h  IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner 23443086
SP6.5 Apoptosis Assay 5 μM 24 h  induces apoptosis  23443086
VUP Apoptosis Assay 5 μM 24 h  induces apoptosis  23443086
OCM1 Apoptosis Assay 5 μM 24 h  induces apoptosis  23443086
OM431 Apoptosis Assay 5 μM 24 h  induces apoptosis  23443086
SP6.5 Function Assay 5 μM 12 h reduces the migration  23443086
VUP Function Assay 5 μM 12 h reduces the migration  23443086
OCM1 Function Assay 5 μM 12 h reduces the migration  23443086
OM431 Function Assay 5 μM 12 h reduces the migration  23443086
HBL-1  Growth Inhibition Assay 3 μM 24/48/72 h DMSO slows cell growth modestly 23441730
RAW 264.7 Function Assay 2-15 μM 1 h DMSO suppresses the activation of IKK family members 23441730
IL-1R  Function Assay 2-15 μM 1 h DMSO suppresses the activation of IKK family members 23441730
RAW 264.7 Function Assay 15 μM 1 h DMSO suppresses the activation of and JNK 23441730
IL-1R  Function Assay 15 μM 1 h DMSO suppresses the activation of and JNK 23441730
U2OS Function Assay 15 μM 1 h DMSO prevents the LPS- or IL-1-stimulated formation of K63-pUb chains  23441730
MT‐1  Function Assay 8 µm 3 h decreases the levels of p‐STAT3 and p‐4EBP1 23278479
MT‐2  Function Assay 8 µm 3 h decreases the levels of p‐STAT3 and p‐4EBP1 23278479
MT‐1  Function Assay 8 µm 3 h decreases the levels of the p65 subunit of NF‐κB  23278479
MT‐2  Function Assay 8 µm 3 h decreases the levels of the p65 subunit of NF‐κB  23278479
MCF-7  Function Assay 2.5-15 μM 0.5 h DMSO causes the gradual loss of cell adhesion 23093227
HaCaT  Function Assay 5.0 μM 1 h  attenuates the TCOH-induced production of IL-6  23041168
A549  Function Assay 1 h inhibits LTA-induced SP-A mRNA production significantly 23031213
OA chondrocytes  Function Assay 10 μM 1 h blocks the AGE-BSA-induced gene/protein expression of GRP78 or COX-2 (p<0.05) 22982228
RAW264.7 Function Assay 15 μM 15-120 min blocks the production of NO, PGE2, and TNF-α 22745523
RAW264.7 Growth Inhibition Assay 5-30 μM 24 h inhibits cell growth in a dose-dependent manner 22745523
HBL6 Apoptosis Assay 0.5/5/25 μM 6/24 h decreases cell viability and leeads to apoptosis in a dose-dependent manner  22074820
HT29  Function Assay 1-10 μM 10 h increases HO-1 mRNA and protein expression 21620964
Ca9–22 Apoptosis Assay 10 μM  1 h completely inhibits ALA-PDT-induced apoptosis 21138480
Ca9–22 Function Assay 10 μM  1 h completely abrogates the ALA-PDT-induced JNK activation 21138480
A-549 Growth Inhibition Assay 10 μM  24/48 h inhibits cell growth in a time-dependent manner 20866043
AP Function Assay 5/10 μM 48 h downregulates the BAD protein level a dose-dependent manner 20596645
AQ1 Function Assay 5/10 μM 48 h downregulates the BAD protein level a dose-dependent manner 20596645
AP Function Assay 20 μM 4/8 h downregulates the BAD protein level a time-dependent manner 20596645
AQ1 Function Assay 20 μM 4/8 h downregulates the BAD protein level a time-dependent manner 20596645
THP-1 Function Assay 5 μM  0.5 h attenuates the LPS-induced p-IκBα protein by 72% 20309718
K562 Growth Inhibition Assay 2-30 μM 24 h IC50=8 μM,inhibits cell growth in a dose-dependent manner 19646807
Jurket Growth Inhibition Assay 2-30 μM 24 h IC50=7.1 μM, inhibits cell growth in a dose-dependent manner 19646807
U937 Growth Inhibition Assay 2-30 μM 24 h IC50=10.5 μM, inhibits cell growth in a dose-dependent manner 19646807
PBMC Growth Inhibition Assay 2-30 μM 24 h IC50=40.2 μM, inhibits cell growth in a dose-dependent manner 19646807
K562 Apoptosis Assay 2-20 μM  24 h induces a dose-dependent apoptosis 19646807
THP1 Cytotoxicity assay 72 hrs Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay, TC50 = 1.5 μM. 28410442
RAW264.7 Function assay 6 hrs Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay, IC50 = 1.72 μM. 24315191
HEK293 Function assay 6 hrs Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM. 24533857
HEK293 Function assay 6 hrs Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM. 24992702
HEK293 Function assay 6 hrs Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM. 26343828
HEK293 Function assay 6 hrs Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM. 22850207
HEK293 Function assay 6 hrs Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay, IC50 = 2.01 μM. 22712432
HEK293 Cytotoxicity assay Cytotoxicity against HEK293 cells, IC50 = 3.8 μM. 24533857
HEK293 Function assay 6 hrs Inhibition of TNFalpha-induced NFkappaB (unknown origin) activation expressed in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 5 μM. 23316950
HEK293 Function assay Effect on Cdc2 expressed in HEK293 cells assessed as effect on Cdc2:Cdc25C interaction complexes in presence of camptothecin by EYFP and/or YFP Venus fragment based reporter gene assay 16680159
HEK293 Function assay 20 uM 24 hrs Inhibition of TNF-alpha stimulated NFkappaB transactivation in HEK293 cells at 20 uM measured after 24 hrs by dual luciferase reporter gene assay 27736063
RAW264.7 Function assay 20 uM 1 hr Inhibition of LPS-induced NFkB activation in mouse RAW264.7 cells assessed as reduction in nuclear translocation of p65 at 20 uM preincubated for 1 hr followed by LPS stimulation measured after 3 hrs by Western blot method 28667873
RAW264.7 Function assay 20 uM 6 hrs Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells at 20 uM treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay 24315191
RAW264.7 Antinflammatory assay 20 uM 18 hrs Antinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 20 uM treated 30 mins before LPS challenge measured after 18 hrs by Griess assay 24315191
THP1 Antinflammatory assay 5 uM 24 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced extracellular IL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA 24400858
THP1 Antinflammatory assay 5 uM 24 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced extracellular TNF-alpha production at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA 24400858
THP1 Antinflammatory assay 5 uM 24 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced intracellular proIL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA 24400858
THP1 Antinflammatory assay 5 uM 24 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced intracellular IL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA 24400858
RAW264.7 Function assay 0.3 ug/ml 12 hrs Inhibition of LPS-induced NF-kB p65 phosphorylation in mouse RAW264.7 cells at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method 28284806
RAW264.7 Function assay 0.3 ug/ml 12 hrs Inhibition of LPS-induced NF-kB p65 activation in mouse RAW264.7 cells at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by DAPI staining based inverted fluorescence microscopic method 28284806
RAW264.7 Function assay 0.3 ug/ml 12 hrs Inhibition of NF-kB p65 in mouse RAW264.7 cells assessed as reduction in LPS-induced iNOS expression at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method 28284806
RAW264.7 Function assay 0.3 ug/ml 12 hrs Inhibition of NF-kB p65 in mouse RAW264.7 cells assessed as reduction in LPS-induced COX2 expression at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method 28284806
HEK293 Function assay 20 uM 24 hrs Inhibition of TNFalpha-induced NFkappaB activation in HEK293 cells at 20 uM after 24 hrs by dual luciferase reporter gene assay 28873303
RAW264.7 Function assay 20 uM 2 hrs Inhibition of NFkappaB nuclear translocation in LPS-stimulated mouse RAW264.7 cells at 20 uM pretreated for 2 hrs followed by LPS-induction by DAPI-staining based immunofluorescence microscopic method 29759725
BGC823 Function assay 5 uM 12 hrs Inhibition of colony formation in human BGC823 cells at 5 uM treated for 12 hrs followed by incubation in drug free medium for 14 days by crystal violet staining based assay 28881286
SGC7901 Function assay 5 uM 12 hrs Inhibition of colony formation in human SGC7901 cells at 5 uM treated for 12 hrs followed by incubation in drug free medium for 14 days by crystal violet staining based assay 28881286
RAW264.7 Function assay 10 uM 2 hrs Inhibition of LPS-induced IL-6 mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method 27038497
RAW264.7 Function assay 10 uM 2 hrs Inhibition of LPS-induced IL-1beta mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method 27038497
RAW264.7 Function assay 10 uM 2 hrs Inhibition of LPS-induced iNOS mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method 27038497
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Biological Activity

Description BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.
Targets
E2-conjugating enzymes [6]
(Cell-free assay)		 USP7 [7]
(Cell-free assay)		 USP21 [7]
(Cell-free assay)		 USP6 [7]
(Cell-free assay)		 IκBα phosphorylation [1]
(Tumor cells)
0.19 μM 0.96 μM 1.7 μM 10 μM
In vitro
In vitro

BAY 11-7082 completely and specifically abrogates NF-κB DNA binding, downregulating the NF-κB-inducible cytokine IL-6 and inducing apoptosis. [1]

BAY 11-7082 (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. BAY 11-7082 (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. [2]

Bay 11-7082 (5 μM) rapidly and efficiently reduces the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-x(L), whereas it has little effect on the DNA binding of another transcription factor, AP-1. Bay 11-7082-induced apoptosis of primary ATL cells is more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells is also associated with down-regulation of NF-kappaB activity. Bay 11-7082 (5 μM) selectively induces apoptosis of HTLV-I–infected T-cell lines associated with down-regulation of the expression of cyclin D1, cyclin D2, and Bcl-xL. [3]

BAY 11-7082 (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. BAY 11-7082 prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. [4]

BAY 11-7082 at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, BAY 11-7082 at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. BAY 11-7082 (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. BAY 11-7082 (100 μM) significantly decreases the release of TNF-α from adipose tissue, whereas the release of IL-6 and IL-8 is significantly inhibited at all concentrations of BAY 11-7082 tested. BAY 11-7082 (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. [5]

BAY 11-7082 is also found to inactivate the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), and thus induces B-cell lymphoma and leukaemic T-cell death. [6]
Cell Research Cell lines NCI-H1703 cells
Concentrations ~8 μM
Incubation Time 12 hours
Method

Cells are transfected with siRNA in 96-well microtiter plates and then cultured for 72 hours in complete NSCLC medium, treated with BAY 11-7082 for 12 hours. Cells are incubated with [3H]thymidine for 3 hours. The cells are collected on filters using an automatic cell harvester and radioactivity on the filters is measured by β-scintillation counting.
Experimental Result Images Methods Biomarkers Images PMID
Western blot NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4 NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4 31332209
Growth inhibition assay Cell viability Cell viability 31332209
In Vivo
In vivo

BAY 11-7082, an NF-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells.
Animal Research Animal Models Male BALB/c nude mice
Dosages 2.5 & 5 mg/kg
Administration i.t.

Chemical lnformation & Solubility

Molecular Weight 207.25 Formula

C10H9NO2S
CAS No. 19542-67-7 SDF Download BAY 11-7082 SDF
Smiles CC1=CC=C(C=C1)S(=O)(=O)C=CC#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 41 mg/mL ( (197.82 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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